The invention concerns a method for preparing an effervescent granulate including Carnitine an effervescent granulate made accordingly, and its utilization.
The desirable addition of the vitaminlike compound L-Carnitine which plays an important part in the human metabolism, to obtain effervescent granulates, is not practicable due to the high hygroscopicity of this substance, up to the present time. L-Carnitine performs an essential function for the utilization of fatty acids and for the transport of metabolic energy.
The betaine character, that is the formation of an internal salt between the positively charged nitrogen and the negatively charged COO group in Carnitine is the reason for its ability to react on acids and its high hygroscopicity. Therefore, the commercially available pharmaceutical Carnitine preparations mix Carnitine with inert substances in order to prevent the possibilities of reaction. Mainly inert substances have also been suggested for tablet pressing. However, due to the volume it is hardly any longer possible to use large dosages such as for example the oral administration of e.g. 1 g of Carnitine in the form of a tablet. Also a dilution with sugar, carbohydrates and other inert substances for the purpose of establishing a base for preparing a drinking solution results in too large a volume total and too high weights. This base is not acceptable in terms of taste and not economical.
But efforts are made to dissolve these large dosages in water before taking the preparation.
But this modern form of administration designed for larger dosages of active pharmaceutical substances should dissolve fast and in the form of a tasty beverage. However, such preparations require, as is known, an acceptable taste, besides a fast dissolution, due to organic acids of the type of tartaric acid, citric acid, malic acid etc. as well as carbonates or bicarbonates of the type of sodium carbonate, calcium carbonate etc.
When L-Carnitine comes into contact with organic acids, acid salts are formed, as described in the EP-0-0 150 688, which are said to have a by far lower hygroscopicity than L-Carnitine proper. However, these acid salts must now be insulated at this stage, because otherwise they will continue to react with the organic acid finally resulting in a glassy still much more hygroscopic structure than the L-Carnitin proper.